•Corticosteroid—Anti-inflammatory
•Indication: Asthma (first line treatment for persistent, chronic asthma.) Steroids are not effective in COPD, which involves an immediate TH1 mediated response.
•MOA: inhibit the inflammatory response by: (1) preventing the production & release of inflammatory mediators and (2) inducing apoptosis in eosinophils & TH2 lymphocytes. Overall effect is suppression of the inflammatory response and a reduction in airway hyperresponsiveness, but not a cure of the underlying disease. Lung damage from airway remodeling is not reversed by steroid use.
•Dosing/Admin: low (2 puffs 2x/day), medium (2 puffs 4x/day), high (4puffs 4x/day).
Use the lowest dose that will control symptoms. High doses increase the risk of systemic absorption.
Because this is steroidal, it will take days to become fully effective. Not for immediate relief.
•Side Effects: thrush (oropharyngeal yeast infection), dysphonia (hoarseness). Incidence of side effects is reduced by using a spacer & by rinsing mouth after taking drug.

51. Methylpredisolone (Solu-Medrol)

•Corticosteroid: Oral or parenteral steroid
•Example: Solu-Medrol
•Indication: some cases of severe persistent asthma; can consider for short term use (5-10 days) during exacerbations in all patients—fewer side effects w/ short term use.
•MOA:
Dosing: effects occur in 6-12 h.
•Admin precautions: long term use can cause adrenal suppression, so do not stop treatment suddenly. Patient must be weaned slowly.
•Side Effects: ↑BP, ↑ diabetes, ↑risk of infections, weight gain, osteoporosis, cataracts, facial swelling, Cushingoid habitus.

52. Zafirlukast/Montelukast

•Leukotriene Receptor Antagonist
•Example: Zafirlukast (Accolate) (2x/day)
Montelukast (Singulaire) (1x/day)
•Indication: chronic use in mild to moderate asthma usually in combination with inhaled steroid; addition of a leukotriene modifer may allow for a reduction in the dose of inhaled steroid.
•MOA: blocks leukotriene receptors preventing all deleterious effects mediated by leukotrienes (bronchoconstriction, chemotaxis of inflammatory cells, mucous production, increased vascular permeability). Receptors are on smooth muscle.
•Dose/Admin: available for oral use only.

•Β1 antagonist w/ intrinsic sympathomimetic activity (ISA) = PARTIAL AGONIST
•Indication: hypertension in patients with bradycardia (low HR)
•MOA: β1 and β2 receptors are partially activated, but unable to respond to more potent catecholamines.
•Side Effects: Because of ISA, it is less likely to cause bradycardia in patients with hypertension & low HR (athletes). It doesn’t always slow the HR @ rest as much as other β blockers, but it still blocks an increase in HR & CO produced by the SNS.